PH12018501643A1 - Tlr7 agonist crystalline form a, preparation method and use thereof - Google Patents

Tlr7 agonist crystalline form a, preparation method and use thereof

Info

Publication number
PH12018501643A1
PH12018501643A1 PH12018501643A PH12018501643A PH12018501643A1 PH 12018501643 A1 PH12018501643 A1 PH 12018501643A1 PH 12018501643 A PH12018501643 A PH 12018501643A PH 12018501643 A PH12018501643 A PH 12018501643A PH 12018501643 A1 PH12018501643 A1 PH 12018501643A1
Authority
PH
Philippines
Prior art keywords
crystalline form
preparation
tlr7 agonist
tlr7
agonist
Prior art date
Application number
PH12018501643A
Inventor
Zhaozhong Ding
Fei Sun
Yinghu Hu
Yilong Zhou
Zheng Wang
Rui Zhao
Ling Yang
Original Assignee
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chia Tai Tianqing Pharmaceutical Group Co Ltd filed Critical Chia Tai Tianqing Pharmaceutical Group Co Ltd
Publication of PH12018501643A1 publication Critical patent/PH12018501643A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.
PH12018501643A 2016-02-05 2018-08-02 Tlr7 agonist crystalline form a, preparation method and use thereof PH12018501643A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610082029.8A CN107043379A (en) 2016-02-05 2016-02-05 A kind of crystal formation A, its preparation method and the medical usage of TLR7 activators
PCT/CN2017/072891 WO2017133684A1 (en) 2016-02-05 2017-02-04 Tlr7 agonist crystalline form a, preparation method and use thereof

Publications (1)

Publication Number Publication Date
PH12018501643A1 true PH12018501643A1 (en) 2019-06-03

Family

ID=59499348

Family Applications (1)

Application Number Title Priority Date Filing Date
PH12018501643A PH12018501643A1 (en) 2016-02-05 2018-08-02 Tlr7 agonist crystalline form a, preparation method and use thereof

Country Status (28)

Country Link
US (2) US10442811B2 (en)
EP (1) EP3412672B1 (en)
JP (1) JP6889171B2 (en)
KR (1) KR102393280B1 (en)
CN (2) CN107043379A (en)
AR (1) AR107548A1 (en)
AU (1) AU2017215801B2 (en)
BR (1) BR112018015880A2 (en)
CA (1) CA3013518C (en)
CL (1) CL2018002092A1 (en)
DK (1) DK3412672T3 (en)
EA (1) EA035951B1 (en)
ES (1) ES2830443T3 (en)
HK (1) HK1259170A1 (en)
HR (1) HRP20201644T1 (en)
HU (1) HUE051399T2 (en)
IL (1) IL260968B (en)
LT (1) LT3412672T (en)
MX (1) MX2018009501A (en)
NZ (1) NZ744884A (en)
PH (1) PH12018501643A1 (en)
PL (1) PL3412672T3 (en)
PT (1) PT3412672T (en)
SG (1) SG11201806683UA (en)
SI (1) SI3412672T1 (en)
TW (1) TWI754629B (en)
UA (1) UA121161C2 (en)
WO (1) WO2017133684A1 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA44334A (en) 2015-10-29 2018-09-05 Novartis Ag ANTIBODY CONJUGATES INCLUDING A TOLL-TYPE RECEPTOR AGONIST
CN107043379A (en) * 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 A kind of crystal formation A, its preparation method and the medical usage of TLR7 activators
CN107043378A (en) * 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 A kind of Preparation Method And Their Intermediate of pyrrolo- [3,2-d] pyrimidines
CN107043380A (en) 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 A kind of maleate of TLR7 activators, its crystal formation C, crystal formation D, crystal formation E, preparation method and purposes
AU2019272478A1 (en) * 2018-05-25 2020-12-17 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. TLR7 agonist and pharmaceutical combination thereof for treating lung cancer
WO2020162705A1 (en) 2019-02-08 2020-08-13 성균관대학교산학협력단 Toll-like receptor 7 or 8 agonist-cholesterol complex, and use of same
US20220249488A1 (en) * 2019-03-15 2022-08-11 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Toll-like receptor agonists for use in the treatment of hepatitis b
CA3137202A1 (en) * 2019-04-23 2020-10-29 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Solid pharmaceutical composition comprising tlr7 agonist
CA3170551A1 (en) 2020-03-02 2021-09-10 Yong Taik Lim Live-pathogen-mimetic nanoparticles based on pathogen cell wall skeleton, and production method thereof
EP4194006A1 (en) 2020-08-04 2023-06-14 Progeneer Inc. Mrna vaccine comprising adjuvant capable of kinetic control
EP4194008A1 (en) 2020-08-04 2023-06-14 Progeneer Inc. Kinetically acting adjuvant ensemble
JP2023536954A (en) 2020-08-04 2023-08-30 プロジェニア インコーポレイテッド Conjugate of Toll-like Receptor 7 or 8 Agonist with Temporarily Inactivated Activation Site and Functional Drug, and Use of the Same

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3376479B2 (en) * 1991-08-12 2003-02-10 武田薬品工業株式会社 Condensed pyrimidine derivatives, their production and use
EP1931352B1 (en) * 2005-08-22 2016-04-13 The Regents of The University of California Tlr agonists
KR101787309B1 (en) 2008-12-09 2017-10-18 길리애드 사이언시즈, 인코포레이티드 Modulators of toll-like receptors
US9139590B2 (en) * 2011-02-04 2015-09-22 Duquesne University Of The Holy Spirit Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity and methods of treating a patient
WO2013103967A1 (en) * 2012-01-05 2013-07-11 Northeastern University Allosteric modulators of cb1 cannabinoid receptors
HUE037064T2 (en) * 2012-10-10 2018-08-28 Janssen Sciences Ireland Uc Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
US9550785B2 (en) 2012-11-20 2017-01-24 Glaxosmithkline Llc Pyrrolopyrimidines as therapeutic agents for the treatment of diseases
ES2625023T3 (en) * 2012-11-20 2017-07-18 Glaxosmithkline Llc Novel compounds
HUE13857477T2 (en) * 2012-11-20 2018-05-28 Glaxosmithkline Llc Novel compounds
EA030603B1 (en) 2014-05-01 2018-08-31 Новартис Аг COMPOUNDS AND COMPOSITIONS AS Toll-LIKE RECEPTOR 7 AGONISTS
UA117634C2 (en) 2014-08-15 2018-08-27 Чиа Тай Тяньцін Фармасьютикал Ґруп Ко., Лтд. Pyrrolopyrimidine compounds used as tlr7 agonist
CN105367576A (en) 2014-08-15 2016-03-02 正大天晴药业集团股份有限公司 Pyrrolopyrimidine compounds as TLR7 agonists
CN107043379A (en) * 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 A kind of crystal formation A, its preparation method and the medical usage of TLR7 activators
CN107043380A (en) 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 A kind of maleate of TLR7 activators, its crystal formation C, crystal formation D, crystal formation E, preparation method and purposes

Also Published As

Publication number Publication date
US10947245B2 (en) 2021-03-16
HUE051399T2 (en) 2021-03-01
WO2017133684A1 (en) 2017-08-10
CN108602831A (en) 2018-09-28
NZ744884A (en) 2022-09-30
US20200039988A1 (en) 2020-02-06
KR102393280B1 (en) 2022-05-02
CN108602831B9 (en) 2020-12-04
JP2019505533A (en) 2019-02-28
ES2830443T3 (en) 2021-06-03
DK3412672T3 (en) 2020-10-19
CA3013518C (en) 2022-07-19
KR20180104117A (en) 2018-09-19
US20190040071A1 (en) 2019-02-07
HK1259170A1 (en) 2019-11-29
CN108602831B (en) 2020-11-03
PT3412672T (en) 2020-11-11
TWI754629B (en) 2022-02-11
BR112018015880A2 (en) 2018-12-26
AR107548A1 (en) 2018-05-09
LT3412672T (en) 2020-11-10
JP6889171B2 (en) 2021-06-18
CL2018002092A1 (en) 2018-12-07
SI3412672T1 (en) 2021-02-26
MX2018009501A (en) 2018-12-11
TW201728589A (en) 2017-08-16
SG11201806683UA (en) 2018-09-27
US10442811B2 (en) 2019-10-15
IL260968B (en) 2022-05-01
EP3412672A1 (en) 2018-12-12
AU2017215801A1 (en) 2018-08-23
EP3412672B1 (en) 2020-07-15
UA121161C2 (en) 2020-04-10
EP3412672A4 (en) 2019-07-17
AU2017215801B2 (en) 2020-09-10
EA035951B1 (en) 2020-09-04
HRP20201644T1 (en) 2020-12-25
CN107043379A (en) 2017-08-15
PL3412672T3 (en) 2021-01-25
EA201891768A1 (en) 2019-01-31
CA3013518A1 (en) 2017-08-10

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